title: Ruthenium(II) polypyridyl complexes: synthesis and studies of DNA binding, photocleavage, cytotoxicity, apoptosis, cellular uptake, and antioxidant activity.
abstract: Two ruthenium (II) complexes [Ru(dmb)2(APIP)](ClO4)2 (APIP=2-(2-aminophenyl)imidazo[4,5-f ][1,10]phenanthroline, dmb=4,4'-dimethyl-2,2'-bipyridine; 1) and [Ru(dmb)2(HAPIP)](ClO4)2 (HAPIP=2-(2-hydroxyl-4-aminophenyl)imidazo[4,5-f ][1,10]phenanthroline; 2) were synthesized and characterized. DNA binding was investigated by electronic absorption titration, luminescence spectra, thermal denaturation, viscosity measurements, and photocleavage. The DNA binding constants for complexes 1 and 2 were 4.20 (±0.14)×10(4) and 5.45 (±0.15)×10(4) M(-1). The results suggest that these complexes partially intercalate between the base pairs. The cytotoxicity of complexes 1 and 2 was evaluated by MTT assay. Cellular uptake was observed under fluorescence microscopy; complexes 1 and 2 can enter into the cytoplasm and accumulate in the nuclei. Apoptosis and the antioxidant activity against hydroxyl radicals (•OH) were also explored.
authors.affiliation: School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou, PR China. lyjche@163.com
authors.forename: Yun-Jun
authors.initials: YJ
authors.lastname: Liu
authors.forename: Zhen-Hua
authors.initials: ZH
authors.lastname: Liang
authors.forename: Zheng-Zheng
authors.initials: ZZ
authors.lastname: Li
authors.forename: Jun-Hua
authors.initials: JH
authors.lastname: Yao
authors.forename: Hong-Liang
authors.initials: HL
authors.lastname: Huang
mesh_terms: D015082:2,2'-Dipyridyl / Q000737:chemistry; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D000975:Antioxidants / Q000138:chemical synthesis / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology; D045744:Cell Line, Tumor; D002467:Cell Nucleus / Q000378:metabolism; D002470:Cell Survival / Q000187:drug effects / Q000528:radiation effects; D004247:DNA / Q000737:chemistry / Q000378:metabolism*; D024202:Electrophoretic Mobility Shift Assay; D005260:Female; D005453:Fluorescence; D006801:Humans; D017665:Hydroxyl Radical / Q000037:antagonists & inhibitors / Q000378:metabolism; D007364:Intercalating Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D007700:Kinetics; D008113:Liver Neoplasms / Q000188:drug therapy / Q000473:pathology; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D010084:Oxidation-Reduction / Q000187:drug effects / Q000528:radiation effects; D010618:Phenanthrolines / Q000737:chemistry; D010782:Photolysis / Q000528:radiation effects; D010957:Plasmids / Q000378:metabolism; D012428:Ruthenium / Q000737:chemistry / Q000378:metabolism*; D013057:Spectrum Analysis; D014466:Ultraviolet Rays
chemical_list: D000970:Antineoplastic Agents; D000975:Antioxidants; D007364:Intercalating Agents; D009942:Organometallic Compounds; D010618:Phenanthrolines; D017665:Hydroxyl Radical; D015082:2,2'-Dipyridyl; D012428:Ruthenium; D004247:DNA; C427203:calf thymus DNA